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Opioid Analgesics: Chemistry and Receptors, by A.F. Casy, R.T. Parfitt
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The rapidly burgeoning research of the past two decades on agonist-antagonist analgesics and opioid receptors makes this exhaustive review of opioid anal gesics particularly relevant and timely. After an introductory chapter the additional 12 chapters begin logically with morphine and congeners (4- epoxymorphinans) and end with opioid receptors. All principal chemical types of centrally acting analgesics (including endogenous opioid-like substances) and their antagonists as well as the mixed agonist-antagonists are treated thoroughly, although not always (and for good reason) in historical (chrono logical) order. A chapter on miscellaneous types (atypical structures for the most part) includes the benzimidazoles (etonitazene), aminotetralins (dezocine), tetrahydroisoquinolines (methopholine), and so on. Important aspects and correlations of chemistry, pharmacology, and biochemistry are discussed in depth. Literature citations are numerous. For educators, practicing laboratory scientists, and physicians, this scholarly review by two authors well of opioid analgesics versed in the chemistry, pharmacology, and biochemistry will be informative, stimulating, and thought-provoking. Everette L. May Medical College of Virginia Richmond, VA 23298 v Preface The history of opium predates the written word, although knowledge of its constituents dates back less than 200 years. Over the centuries its popularity for the relief of pain has waxed and waned, until today the opiates are widely recognized as excellent analgesics but with disadvantages that have impaired their use seriously. There is a clear need for a potent analgesic with minimal effects on the respiratory centers and gastrointestinal tract and preferably devoid of dependence liability.
- Sales Rank: #3728913 in Books
- Published on: 1986-06-30
- Original language: English
- Number of items: 1
- Dimensions: 9.21" h x 1.25" w x 6.14" l, 2.04 pounds
- Binding: Hardcover
- 518 pages
Most helpful customer reviews
3 of 3 people found the following review helpful.
Quintessential Review of the Chemistry & Pharmacology of Opioid Analgesics
By Jonathan Berry
Quintessential Review of the Chemistry & Pharmacology of Opioid Analgesics
This comprehensive, thoroughly referenced treatment of opioid analgesics is relevant and applicable even today (25 years after its publication), given the rapidly burgeoning research of the past 40+ years on agonist-antagonist analgesics and opioid receptors. The authors have surpassed their stated aim, "to afford medicinal scientists an entry into the chemistry and biological activity of morphine and related compounds."
Very few researchers are more qualified to review the 100+ years of opioid chemistry/pharmacology than the authors of this title, Alan F. Casy and Robert T. Parfitt. A. F. Casy has dedicated his entire 60+ year career to the field of opioid research and has published hundreds of papers in the peer-reviewed literature during this time. R. T. Parfitt has dedicated much of his career to the study of opioids as well. At the time this book was published, I can think of only a few other researchers who were equally qualified to author such a comprehensive review. These include some of the heaviest hitters in the opioid research community, such as Philip S. Portoghese, Nathan B. Eddy, Kenneth W. Bentley, Everette L. May, Paul A.J. Janssen, and Daniel Lednicer.
An introductory chapter that briefly covers definitions, testing methods, side effects, pharmacokinetics, and biochemical and bibliographical aspects is followed by 4,5-Epoxymorphinans, not surprisingly, the most extensive chapter of the book. Chapters 3-5, concerned with, respectively, morphinans, benzomorphans, and the interesting but little-investigated 5-arylmorphans, follow logically for reasons of genesis and structural similarities. The next three chapters treat piperidine-type analgesics (pethidine and related 4-phenylpiperidine analgesics-6; further analgesics based on piperidine and related azabicycloalkanes: prodines, promedols, profadol, and their derivatives-7; fentanyl and the 4-anilinopiperidino group of analgesics-8). Methadone and related 3,3-diphenylpropylamines constitute Chapter 9 while enkephalins, endorphins, and other opioid peptides are given good coverage in Chapter 10. Chapter 11 deals with miscellaneous groups of analgesics (atypical structural types, e.g., benzimidazoles, tetrahydroisoquinolines, arylcyclohexylamines, aminotetralins, etc.). The final two chapters on antagonists, dualists (agonist-antagonists), and Kappa agonists (12) and opioid receptors (13) are particularly scholarly and should evoke widespread interest. Throughout, molecular geometry (especially optical isomerism) and structure-activity analyses and interrelationships are emphasized.
Major criticisms of the book are the lack of coverage of non-Mu opioids and the price. Coverage of opioid ligands acting at the Kappa and Delta opioid receptors was lacking. Only a single 39-page chapter was devoted to topics such as partial opioid agonist-antagonists, antagonists, dualists and Kappa agonists. With partial agonist-antagonists, mixed agonists, and Delta/Kappa ligands comprising a significant portion of opioid research over the past 25+ years, it is surprising that so little content was devoted to such topics. As far as the price is concerned, for a 540-page book, a list price of $299 is unreasonable. As a result, I have posted a free eBook version of this book on Scribd. The URL link to the eBook is listed below:
[...]
Minor criticisms are the use of 3-benzazocine numbering with the 6,7-benzomorphan generic name (Chapter 4) and the limiting subtitle of the book which could better have been "Chemistry, Pharmacology and Receptors."
For educators, students, research scientists, and physicians interested in centrally acting pain-relieving agents, this book by two authors well versed in the chemistry, pharmacology, and biochemistry of opioid analgesics will be informative, stimulating, and thought-provoking.
For those involved or simply interested in opioid research, I have compiled a brief listing of the top 8 most important texts dealing with the chemistry & pharmacology of opioids.
(1) Opioid Analgesics: Chemistry and Receptors - Alan F. Casy and Robert T. Parfitt - Plenum Press (1986) - ISBN-10: 0306421305 - ISBN-13: 9780306421303
(2) Opiates - George R. Lenz, Suzanne M. Evans, D. Eric Walters, and Anton J. Hopfinger - Academic Press (1986) - ISBN: 012443830X
(3) Central Analgetics - Chemistry and Pharmacology of Drugs, A Series of Monographs, Vol. 1 - Daniel Lednicer (editor) - Wiley-Interscience (1982) - ISBN: 0471083143
(4) Analgesics: From Chemistry and Pharmacology to Clinical Application - Helmut Buschmann, Thomas Christoph, Elmar Friderichs, and Corinna Maul - Wiley-VCH (2002) - ISBN-10: 3527304037 - ISBN-13: 9783527304035
(5) Analgetics - Medicinal Chemistry, A Series of Monographs, Vol. 5 - George deStevens - Academic Press (1965) - Library of Congress Card No. 65-15524
(6) Synthetic Analgesics, Part IIA: Morphinans, Organic Chemistry, Vol. VIII - J. Hellerbach, O. Schnider, H. Besendorf, B. Pellmont - Pergamon Press (1966) - Library of Congress Card No. 59-13814
(7) Synthetic Analgesics, Part IIB: Benzomorphans - International Series of Monographs on Organic Chemistry, Vol. 8 - Nathan B. Eddy and Everette L. May - Pergamon Press (1966) - Library of Congress Card No. 59-13814
(8) Synthetic Analgesics, Part I: Diphenylpropylamines - International Series of Monographs on Organic Chemistry, Vol. 3 - Paul A. J. Janssen - Pergamon Press (1960) - Library of Congress Card No. 59-13814
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